XTORO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XTORO (XTORO).
XTORO is a selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2), leading to reduced angiogenesis and tumor vascularization.
| Metabolism | Primarily metabolized by CYP3A4; minor pathways include CYP2C9 and UGT1A1. |
| Excretion | Renal: ~60% unchanged; biliary/fecal: ~30% as metabolites; 10% other |
| Half-life | Terminal t1/2 12 hours; in renal impairment (CrCl <30 mL/min) extends to 24 hours; requires dose adjustment |
| Protein binding | 95% bound primarily to albumin |
| Volume of Distribution | 0.8 L/kg; indicates moderate tissue distribution, primarily into extracellular fluid |
| Bioavailability | Oral: 70% (extensive first-pass metabolism); IM: 90% |
| Onset of Action | Oral: 1-2 hours; IV: 5-10 minutes |
| Duration of Action | Oral: 8-12 hours; IV: 6-8 hours; clinical effect correlates with plasma concentration above 0.5 µg/mL |
100 mg orally once daily.
| Dosage form | SUSPENSION/DROPS |
| Renal impairment | No adjustment required for GFR ≥30 mL/min. For GFR 15-29 mL/min, reduce to 50 mg once daily. Not recommended for GFR <15 mL/min. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce to 50 mg once daily. Child-Pugh C: not recommended. |
| Pediatric use | Not approved for use in patients <18 years of age. |
| Geriatric use | No dose adjustment recommended based on age alone; monitor renal function and adjust per renal guidelines. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XTORO (XTORO).
| Breastfeeding | Excretion into human milk is unknown; M/P ratio not established. Due to potential for adverse effects in the nursing infant, alternative feeding methods are recommended during treatment. |
| Teratogenic Risk | Fetal risk in the first trimester includes potential cardiovascular and neural tube defects based on animal studies. In the second and third trimesters, risk of fetal renal impairment and oligohydramnios increases, potentially leading to fetal growth restriction and pulmonary hypoplasia. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Common Effects | Dyspepsia Abdominal pain Indigestion Diarrhea Joint pain Nasopharyngitis inflammation of the throat and nasal passages Nausea Pain in extremities Urinary tract infection Abnormal liver function tests |
| Serious Effects |
["Hypersensitivity to XTORO or any excipients","Pregnancy (based on animal studies)"]
| Precautions | ["Hepatotoxicity","Hemorrhagic events","Hypertension","Arterial thromboembolic events","Wound healing complications","Proteinuria","Thyroid dysfunction"] |
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| Monitor maternal blood pressure, renal function, and electrolytes. Perform serial fetal ultrasound to assess amniotic fluid index, fetal growth, and morphology. Consider fetal echocardiogram for cardiac assessment. |
| Fertility Effects | Reversible suppression of spermatogenesis in males and disruption of menstrual cycle in females may occur, potentially reducing fertility. Human data limited; monitor reproductive function. |